Nitroreductase-induced bioorthogonal ligation for prodrug activation: A traceless strategy for cancer-specific imaging and therapy

Unparalleled ease of access to an anti-cancer agent via a traceless enzymatic-bioorthogonal cascade reaction with H2O as the sole byproduct was developed. The specific “turn-on” fluorescence and linear response to cancer-specific NTR enzymes, as well as slight perturbation to normal cells enable the precursor with both efficient cancer-targeted imaging and therapy.